ArticleBritish journal of pharmacology1993
Characterization of propranolol-resistant (-)-[125I]-cyanopindolol binding sites in rat soleus muscle.
Article in British journal of pharmacology, 1993. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed.
- Agonist-induced desensitisation of βBritish journal of pharmacology · 2019Review
- Tissue functions mediated by beta(3)-adrenoceptors-findings and challenges.Naunyn-Schmiedeberg's archives of pharmacology · 2010Article
- Can [I]-Iodocyanopindolol Label β(3)-Adrenoceptors in Rat Urinary Bladder?Frontiers in pharmacology · 2010Article
- Tools to study beta3-adrenoceptors.Naunyn-Schmiedeberg's archives of pharmacology · 2007Review
- Comparison of three radioligands for the labelling of human beta-adrenoceptor subtypes.Naunyn-Schmiedeberg's archives of pharmacology · 2006Article
- The human near-term myometrial beta 3-adrenoceptor but not the beta 2-adrenoceptor is resistant to desensitisation after sustained agonist stimulation.British journal of pharmacology · 2004Article
- Characterization of beta-adrenoceptor mediated smooth muscle relaxation and the detection of mRNA for beta1-, beta2- and beta3-adrenoceptors in rat ileum.British journal of pharmacology · 1999Article
- Characteristics of cyanopindolol analogues active at the beta 3-adrenoceptor in rat ileum.British journal of pharmacology · 1996Article
- Biphasic effects of the beta-adrenoceptor agonist, BRL 37344, on glucose utilization in rat isolated skeletal muscle.British journal of pharmacology · 1996Article
- Expression of beta 3-adrenoceptor mRNA in rat tissues.British journal of pharmacology · 1996Article
- Characterization and localization of atypical beta-adrenoceptors in rat ileum.British journal of pharmacology · 1995Article
- Acute effects of the beta 3-adrenoceptor agonist, BRL 35135, on tissue glucose utilisation.British journal of pharmacology · 1995Article
- Classical and atypical binding sites for beta-adrenoceptor ligands and activation of adenylyl cyclase in bovine skeletal muscle and adipose tissue membranes.British journal of pharmacology · 1994Article
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3 authors.
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Abstract
1. The characteristics of a propranolol-resistant (-)-[125I]-cyanopindolol (CYP) binding site in rat soleus muscle were determined. 2. Saturation studies performed on homogenates of rat soleus muscle showed two phases of (-)-[125I]-CYP binding, a high affinity site (KD1 30.5 +/- 16.3 pM, Bmax 9.4 +/- 1.38 fmol mg-1 protein) and a lower affinity site (KD2 522.5 +/- 29.1 pM, Bmax 62.19 +/- 11.76 fmol mg-1 protein, n = 4). 3. In rat soleus muscle homogenates labelled with (-)-[125I]-CYP (500 pM), (-)-propranolol competition curves were biphasic with pKD values of 8.30 +/- 0.19, and 5.33 +/- 0.08, n = 7. 4. Competition between (-)-[125I]-CYP (500 pM) and (+/-)-tertatolol, (+/-)-nadolol, (+/-)-alprenolol, (+/-)-CYP, and (-) and (+)-pindolol showed that these compounds competed for binding at the propranolol-resistant site with affinities lower than those displayed at typical beta-adrenoceptors. The atypical beta-adrenoceptor agonists BRL 37344, SR58611A and ICI D7114 and the partial agonist (+/-)-CGP 12177 also competed for (-)-[125I]-CYP binding. 5. Stereoselectivity was demonstrated for the stereoisomers of alprenolol and tertalolol. The (-)-isomers of alprenolol and tertalolol had higher affinity than their corresponding (+)-isomers (3.1 and 2.6 fold respectively). These low stereoselectivity values are a characteristic of atypical beta-adrenoceptors. 6. The beta-adrenoceptor agonists, (-)-adrenaline, (-)-isoprenaline and (-)-noradrenaline, all showed lower affinity than the atypical beta-adrenoceptor agonists and competition curves appeared biphasic in nature. 7. These results confirm the presence of a propranolol-resistant (- )-[125I]-CYP binding site in rat soleus muscle. The affinities of the tested compounds at the propranolol-resistant (- )-[125I]-CYP binding site show similarities to their affinities at 'atypical' beta-adrenoceptors in adipocytes and gastrointestinal tissues and at the cloned beta 3-adrenoceptor.
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